Design, synthesis, in silico molecular modelling studies and biological evaluation of novel indole-thiazolidinedione hybrid analogues as potential pancreatic lipase inhibitors was written by George, Ginson;Auti, Prashant S.;Paul, Atish T.. And the article was included in New Journal of Chemistry in 2021.Related Products of 16312-21-3 This article mentions the following:
Pancreatic lipase (PL) is a key enzyme responsible for the digestion of dietary triglycerides; hence its inhibition is considered as a promising target for the management and/or treatment of obesity. A new series of indole-thiazolidinedione (TZD) hybrid analogs were synthesized using a mol. hybridization approach and evaluated for their anti-obesity effects via PL inhibition. The targeted analogs were synthesized via the condensation reaction between various substituted isatin with TZD in the presence of aqueous KOH in methanol. Amongst the synthesized analogs, 7k and 7m exhibited a potential PL inhibitory activity (IC50 – 7.30 and 9.51μM, resp.). Kinetic study of these potent analogs revealed their competitive mode of enzyme inhibition. This fact was confirmed via fluorescence spectroscopy which further suggested the presence of one binding site for the synthesized analogs. Mol. docking of the synthesized analogs was performed using human PL (PDB ID: 1LPB). The obtained MolDock scores were aligned with the in vitro PL inhibitory activity (Pearson’s r = 0.9108, p < 0.05). Moreover, a stable conformation of the 1LPB-ligands suggested the stability of these complexes in the dynamic environment. These studies provided a basis for the potential role of the indole-TZD hybrids in PL inhibition and further optimization might result in the development of new lead candidates for obesity treatment. In the experiment, the researchers used many compounds, for example, 3-Methylthiazolidine-2,4-dione (cas: 16312-21-3Related Products of 16312-21-3).
3-Methylthiazolidine-2,4-dione (cas: 16312-21-3) belongs to thiazolidine derivatives. Thiazolidines undergo hydrolysis to aldehyde and amino thiol under acid or basic aqueous conditions. Thiazolidine and its composites are key components of many natural products and drugs , and are also present in many synthetic compounds such as anticancer, anti-inflammatory, antitubercular, antifungal, antiviral, anti-HIV, cytotoxicity, antitrypanosomal, antinociceptive and anti-hypernociceptive compounds.Related Products of 16312-21-3
Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com